Methylphenidate and Related Topics

Amphetamine

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Strong central nervous system (CNS) stimulant that is used in the treatment of attention deficit hyperactivity disorder (ADHD), narcolepsy, and obesity.

Psychostimulants like methylphenidate and amphetamine are effective in treating ADHD because they increase neurotransmitter activity in these systems.

Ritalin: 20 mg sustained-release (SR) tablets

Overarching term that covers many drugs including those that increase activity of the central nervous system and the body, drugs that are pleasurable and invigorating, or drugs that have sympathomimetic effects.

A chart comparing the chemical structures of different amphetamine derivatives

Roasted coffee beans, a common source of caffeine.

Lines of illicit cocaine, used as a recreational stimulant

The most frequently prescribed stimulants as of 2013 were lisdexamfetamine (Vyvanse), methylphenidate (Ritalin), and amphetamine (Adderall).

People with ADHD may struggle more than others to focus on tasks such as schoolwork, but can maintain an unusually intense level of attention for tasks they find rewarding or interesting

Attention deficit hyperactivity disorder

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Neurodevelopmental disorder characterized by excessive amounts of inattention, hyperactivity, and impulsivity that are pervasive, impairing in multiple contexts, and otherwise age-inappropriate.

The left prefrontal cortex, shown here in blue, is often affected in ADHD.

Percent of people 4–17 ever diagnosed in the US as of 2011

Timeline of ADHD diagnostic criteria, prevalence, and treatment

Methylphenidate and amphetamine or its derivatives are first-line treatments for ADHD as they are considered the most effective pharmaceutical treatments.

The concentration of orexin-A neuropeptides in the cerebrospinal fluid of narcoleptic individuals is usually very low

Narcolepsy

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Long-term neurological disorder that involves a decreased ability to regulate sleep–wake cycles.

Medications used include modafinil, sodium oxybate and methylphenidate.

Dopamine

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Neuromodulatory molecule that plays several important roles in cells.

Dopamine processing in a synapse. After release dopamine can either be taken up again by the presynaptic terminal, or broken down by enzymes.
TH: tyrosine hydroxylase
DOPA: L-DOPA
DAT: dopamine transporter
DDC: DOPA decarboxylase
VMAT: vesicular monoamine transporter 2
MAO: Monoamine oxidase
COMT: Catechol-O-methyl transferase
HVA: Homovanillic acid

Major dopamine pathways. As part of the reward pathway, dopamine is manufactured in nerve cell bodies located within the ventral tegmental area (VTA) and is released in the nucleus accumbens and the prefrontal cortex. The motor functions of dopamine are linked to a separate pathway, with cell bodies in the substantia nigra that manufacture and release dopamine into the dorsal striatum.

Main circuits of the basal ganglia. The dopaminergic pathway from the substantia nigra pars compacta to the striatum is shown in light blue.

Illustration of dopaminergic reward structures

Dopamine HCl preparation, single dose vial for intravenous administration

Cocaine increases dopamine levels by blocking dopamine transporters (DAT), which transport dopamine back into a synaptic terminal after it has been emitted.

Methamphetamine hydrochloride also known as crystal meth

Dopamine can be found in the peel and fruit pulp of bananas.

Cocaine, substituted amphetamines (including methamphetamine), Adderall, methylphenidate (marketed as Ritalin or Concerta), and other psychostimulants exert their effects primarily or partly by increasing dopamine levels in the brain by a variety of mechanisms.

Methamphetamine

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Potent central nervous system (CNS) stimulant that is mainly used as a recreational drug and less commonly as a second-line treatment for attention deficit hyperactivity disorder and obesity.

Desoxyn (Methamphetamine Hydrochloride) 100 tablets.

A 2010 study ranking various illegal and legal drugs based on statements by drug-harm experts. Methamphetamine was found to be the fourth most damaging to society.

This diagram depicts the neuroimmune mechanisms that mediate methamphetamine-induced neurodegeneration in the human brain. The NF-κB-mediated neuroimmune response to methamphetamine use which results in the increased permeability of the blood–brain barrier arises through its binding at and activation of sigma receptors, the increased production of reactive oxygen species (ROS), reactive nitrogen species (RNS), and damage-associated molecular pattern molecules (DAMPs), the dysregulation of glutamate transporters (specifically, EAAT1 and EAAT2) and glucose metabolism, and excessive Ca2+ ion influx in glial cells and dopamine neurons.

This illustration depicts the normal operation of the dopaminergic terminal to the left, and the dopaminergic terminal in the presence of methamphetamine to the right. Methamphetamine reverses the action of the dopamine transporter (DAT) by activating TAAR1 (not shown). TAAR1 activation also causes some of the dopamine transporters to move into the presynaptic neuron and cease transport (not shown). At VMAT2 (labeled VMAT), methamphetamine causes dopamine efflux (release).

Shards of pure methamphetamine hydrochloride, also known as crystal meth

U.S. drug overdose related fatalities in 2017 were 70,200, including 10,333 of those related to psychostimulants (including methamphetamine).

It has been implicated in addictions to alcohol, cannabinoids, cocaine, methylphenidate, nicotine, opioids, phencyclidine, propofol, and substituted amphetamines, among others.

Opioid

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Opioids are substances that act on opioid receptors to produce morphine-like effects.

US. Top line represents the number of benzodiazepine deaths that also involved opioids. Bottom line represents benzodiazepine deaths that did not involve opioids.

INTA: selective agonist of KOR-DOR and KOR-MOR heteromers. Does not recruit β-arrestin II. Antinociceptive devoid of aversion, tolerance, and dependence in mice.

US yearly deaths from all opioid drugs. Included in this number are opioid analgesics, along with heroin and illicit .<ref name=NIDA-deaths/>

US yearly deaths involving other, predominately Fentanyl.<ref name=NIDA-deaths/>

US yearly deaths involving prescription opioids. is a category dominated by illegally acquired fentanyl, and has been excluded.<ref name=NIDA-deaths>Overdose Death Rates. By National Institute on Drug Abuse (NIDA).</ref>

US yearly overdose deaths involving heroin.<ref name=NIDA-deaths/>

Stimulants (e.g. caffeine, modafinil, amphetamine, methylphenidate)

Nootropic

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Nootropics (, or ) (colloquial: smart drugs and cognitive enhancers) are drugs, supplements, and other substances that are claimed to improve cognitive function, particularly executive functions, attention, memory, creativity, or motivation, in healthy individuals.

Hebbian version of the Yerkes–Dodson law

Stimulants such as dimethylamylamine and methylphenidate are used on college campuses and by younger groups.

Novartis

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Swiss-American multinational pharmaceutical corporation based in Basel, Switzerland and

Suffern, New York: one of the Novartis pharmaceutical production facilities in the United States

Novartis India headquarters in HITEC City, Hyderabad

Novartis in Cambridge, Massachusetts in November 2019.

Novartis manufactures the drugs clozapine (Clozaril), diclofenac (Voltaren; sold to GlaxoSmithKline in 2015 deal), carbamazepine (Tegretol), valsartan (Diovan), imatinib mesylate (Gleevec/Glivec), cyclosporine (Neoral/Sandimmune), letrozole (Femara), methylphenidate (Ritalin; production ceased 2020), terbinafine (Lamisil), deferasirox (Exjade), and others.